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Assay Detail

CHEMBL2423364

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at human DOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.
Nair P, Yamamoto T, Largent-Milnes TM, Cowell S, Kulkarni V, Moye S, Navratilova E, Davis P, Ma SW, Vanderah TW, Lai J, Porreca F, Hruby VJ.
Bioorg Med Chem Lett (2013) 23 : 4975 -4978
PubMed 23899615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.14 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2419538 1 9.59
CHEMBL2419542 1 8.96
CHEMBL2419537 1 8.60
CHEMBL2419541 1 8.32
CHEMBL2419539 1 8.26
CHEMBL2419544 1 7.57
CHEMBL2419543 1 7.12
CHEMBL2419540 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2419538 EC50 = 0.26 nM 9.59
CHEMBL2419542 EC50 = 1.1 nM 8.96
CHEMBL2419537 EC50 = 2.5 nM 8.60
CHEMBL2419541 EC50 = 4.8 nM 8.32
CHEMBL2419539 EC50 = 5.5 nM 8.26
CHEMBL2419544 EC50 = 27.0 nM 7.57
CHEMBL2419543 EC50 = 76.0 nM 7.12
CHEMBL2419540 EC50 = 190.0 nM 6.72